Drug intelligence / Profile preview

erdafitinib + fulvestrant + palbociclib

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

This is a combination therapy consisting of three agents—erdafitinib, fulvestrant, and palbociclib—investigated for the treatment of estrogen receptor-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-), fibroblast growth factor receptor (FGFR)-amplified metastatic breast cancer. - **Erdafitinib** is an investigational oral pan-fibroblast growth factor receptor (FGFR) inhibitor that targets FGFR1–4, blocking aberrant FGFR signaling implicated in tumorigenesis. - **Fulvestrant** is a selective estrogen receptor degrader (SERD) that binds to and accelerates degradation of the estrogen receptor, inhibiting ER-mediated signaling pathways critical for hormone-dependent breast cancer cell survival and proliferation. - **Palbociclib** is an orally available small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which are key regulators of cell cycle progression from G1 to S phase; inhibition leads to cell cycle arrest in ER+ breast cancer cells. The combination aims to overcome resistance mechanisms in advanced/metastatic ER+/HER2-/FGFR-amplified breast cancer by simultaneously targeting hormonal signaling, cell cycle progression, and FGFR-driven oncogenic pathways[1][3][4].

02

Targets

FGFR4 (Fibroblast growth factor receptor 4)ESR2 (ERβ)CDK6 (Cyclin-dependent kinase 6)FGFR3 (Fibroblast growth factor receptor 3)GPER1 (G protein-coupled estrogen receptor 1)CDK4 (Cyclin-dependent kinase 4)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)ESR1 (ERα)VEGFR2 (Vascular endothelial growth factor receptor 2)

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